| Camptothecin (CPT) is a naturally occurring alkaloid first isolated from the native Chinese tree Camptotheca acuminata Dence.(Nyssaceae) in1960s. CPT has been paid considerable attention because of its significant anti-tumor activity. Methoxycamptothecin (MeOCPT) is a natural derivative of camptothecin. The research indicated that MeOCPT showed cytotoxic activity to L1210tumor cells. However, MeOCPT has severe side effects, low water-solubility, short half-life in vivo, and poor stability of lactone ring, limiting their clinical applications. Take gathers the lactic acid as to carry the medicine material to prepared MeOCPT-nanoparticles.MeOCPT-nanoparticles were prepared using poly(lactic acid) by an emulsion and solvent evaporation method. The preparation method was optimized. The optimal ratio of MeOCPT to poly(lactic acid) of0.020:1, and the concentration of surfactant of1%were selected. Using the transmission electron microscope to observe a MeOCPT-nanoparticles granule the shape characteristic. Transmission electron microscope, clear, smooth, uniform round particles were observed with a particle size distribution between100-300nm. The drug loading content and encapsulation efficiency was3.10±1.19%and83.57±3.45%respectively, which was determined by a High-performance liquid chromatographic method. The in vitro release study showed sustained release of MeOCPT from nanoparticles,and the cumulative release rate was close to60%, which can achieve the sustained release effect of the expected.The research succeed MeOCPT sustained-release preparations, and achieved expected results of slow-release drug and reduced toxicity, laid the foundation for further study, with a certain application. |
